IL237369B - N-]2-(6-fluoro-h1-indol-3-yl)ethyl]-3-(2, 2, 3, 3- tetrafluoropropoxy) benzylamine in combination with an acetylcholinesterase inhibitor for the treatment of Alzheimer's disease - Google Patents
N-]2-(6-fluoro-h1-indol-3-yl)ethyl]-3-(2, 2, 3, 3- tetrafluoropropoxy) benzylamine in combination with an acetylcholinesterase inhibitor for the treatment of Alzheimer's diseaseInfo
- Publication number
- IL237369B IL237369B IL237369A IL23736915A IL237369B IL 237369 B IL237369 B IL 237369B IL 237369 A IL237369 A IL 237369A IL 23736915 A IL23736915 A IL 23736915A IL 237369 B IL237369 B IL 237369B
- Authority
- IL
- Israel
- Prior art keywords
- tetrafluoropropoxy
- benzylamine
- indol
- fluoro
- disease
- Prior art date
Links
- WGQKYBSKWIADBV-UHFFFAOYSA-N benzylamine Chemical compound NCC1=CC=CC=C1 WGQKYBSKWIADBV-UHFFFAOYSA-N 0.000 title 2
- 229940100578 Acetylcholinesterase inhibitor Drugs 0.000 title 1
- 208000024827 Alzheimer disease Diseases 0.000 title 1
- 239000000544 cholinesterase inhibitor Substances 0.000 title 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 title 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/27—Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Emergency Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261698664P | 2012-09-09 | 2012-09-09 | |
| US201361782084P | 2013-03-14 | 2013-03-14 | |
| PCT/EP2013/068516 WO2014037532A1 (en) | 2012-09-09 | 2013-09-06 | Methods of treating alzheimer's disease and pharmaceutical compositions thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IL237369A0 IL237369A0 (en) | 2015-04-30 |
| IL237369B true IL237369B (en) | 2018-11-29 |
Family
ID=49118521
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL237369A IL237369B (en) | 2012-09-09 | 2015-02-23 | N-]2-(6-fluoro-h1-indol-3-yl)ethyl]-3-(2, 2, 3, 3- tetrafluoropropoxy) benzylamine in combination with an acetylcholinesterase inhibitor for the treatment of Alzheimer's disease |
Country Status (33)
| Country | Link |
|---|---|
| US (4) | US9375418B2 (lt) |
| EP (1) | EP2892563B1 (lt) |
| JP (2) | JP6693744B2 (lt) |
| KR (2) | KR102342127B1 (lt) |
| CN (1) | CN104619344A (lt) |
| AP (1) | AP2015008306A0 (lt) |
| AU (1) | AU2013311573B2 (lt) |
| BR (1) | BR112015005117B1 (lt) |
| CA (1) | CA2883751C (lt) |
| CL (1) | CL2015000578A1 (lt) |
| CY (1) | CY1121062T1 (lt) |
| DK (1) | DK2892563T3 (lt) |
| EA (1) | EA030448B1 (lt) |
| ES (1) | ES2703630T3 (lt) |
| GE (1) | GEP201706776B (lt) |
| HK (1) | HK1212217A1 (lt) |
| HR (1) | HRP20182069T1 (lt) |
| IL (1) | IL237369B (lt) |
| JO (1) | JO3459B1 (lt) |
| LT (1) | LT2892563T (lt) |
| MX (1) | MX368305B (lt) |
| MY (1) | MY182539A (lt) |
| NI (1) | NI201500031A (lt) |
| NZ (1) | NZ630589A (lt) |
| PL (1) | PL2892563T3 (lt) |
| PT (1) | PT2892563T (lt) |
| RS (1) | RS58104B1 (lt) |
| RU (1) | RU2675786C2 (lt) |
| SG (1) | SG11201501774QA (lt) |
| SI (1) | SI2892563T1 (lt) |
| TN (1) | TN2015000076A1 (lt) |
| TW (1) | TWI632909B (lt) |
| WO (1) | WO2014037532A1 (lt) |
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| CN1826322B (zh) | 2003-07-22 | 2012-04-18 | 艾尼纳制药公司 | 用于预防和治疗相关病症而作为5-ht2a血清素受体调节剂的二芳基和芳基杂芳基脲衍生物 |
| EP2508177A1 (en) | 2007-12-12 | 2012-10-10 | Glaxo Group Limited | Combinations comprising 3-phenylsulfonyl-8-piperazinyl-1yl-quinoline |
| US20110021538A1 (en) | 2008-04-02 | 2011-01-27 | Arena Pharmaceuticals, Inc. | Processes for the preparation of pyrazole derivatives useful as modulators of the 5-ht2a serotonin receptor |
| WO2010062321A1 (en) | 2008-10-28 | 2010-06-03 | Arena Pharmaceuticals, Inc. | Processes useful for the preparation of 1-[3-(4-bromo-2-methyl-2h-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)-urea and crystalline forms related thereto |
| JO3459B1 (ar) * | 2012-09-09 | 2020-07-05 | H Lundbeck As | تركيبات صيدلانية لعلاج مرض الزهايمر |
| WO2014152589A1 (en) | 2013-03-14 | 2014-09-25 | Janssen Pharmaceutica Nv | P2x7 modulators |
| EA029052B1 (ru) | 2013-03-14 | 2018-02-28 | Бёрингер Ингельхайм Интернациональ Гмбх | Замещенные (бензилцианометил)амиды 2-азабицикло[2.2.1]гептан-3-карбоновых кислот в качестве ингибиторов катепсина с |
| JP6467404B2 (ja) | 2013-03-14 | 2019-02-13 | ヤンセン ファーマシューティカ エヌ．ベー． | Ｐ２ｘ７モジュレーター |
| TWI627174B (zh) | 2013-03-14 | 2018-06-21 | 比利時商健生藥品公司 | Ｐ２ｘ７調控劑 |
| TWI599567B (zh) | 2013-03-14 | 2017-09-21 | 健生藥品公司 | Ｐ２ｘ７調節劑 |
| JO3639B1 (ar) * | 2014-07-04 | 2020-08-27 | H Lundbeck As | صورة متعددة الشكل جديدة لـ n-[2-(6-فلورو-1h-إندول-3-يل)إيثيل]-3-(2،2،3،3-تترا فلورو بروبوكسي)بنزيل أمين هيدروكلوريد |
| AP2017009733A0 (en) | 2014-09-12 | 2017-02-28 | Boehringer Ingelheim Int | Spirocyclic inhibitors of cathepsin c |
| US10150766B2 (en) | 2014-09-12 | 2018-12-11 | Janssen Pharmaceutica Nv | P2X7 modulators |
| CN105175307A (zh) * | 2014-11-18 | 2015-12-23 | 苏州晶云药物科技有限公司 | Lu AE58054的盐酸盐晶型A及其制备方法和用途 |
| CA2985366A1 (en) * | 2015-05-07 | 2016-11-10 | Axovant Sciences Gmbh | Methods of treating a neurodegenerative disease |
| AU2016276966A1 (en) | 2015-06-12 | 2018-01-18 | Axovant Sciences Gmbh | Diaryl and arylheteroaryl urea derivatives useful for the prophylaxis and treatment of REM sleep behavior disorder |
| TW201720439A (zh) | 2015-07-15 | 2017-06-16 | Axovant Sciences Gmbh | 用於預防及治療與神經退化性疾病相關的幻覺之作為５－ｈｔ２ａ血清素受體的二芳基及芳基雜芳基脲衍生物 |
| RU2742173C2 (ru) * | 2016-04-26 | 2021-02-02 | Х. Лундбекк А/C | Применение ингибитора ацетилхолинэстеразы и идалопирдина для снижения риска падений у пациентов с болезнью паркинсона |
| US10864191B2 (en) | 2016-05-11 | 2020-12-15 | H. Lundbeck A/S | 5-HT6 receptor antagonists for use in the treatment of Alzheimer's disease with apathy as comorbidity |
| US11458135B2 (en) | 2016-05-18 | 2022-10-04 | Suven Life Sciences Limited | Combination of pure 5-HT6 receptor antagonists with acetylcholinesterase inhibitors |
| CN106309436A (zh) * | 2016-07-25 | 2017-01-11 | 宁波大学 | 可用作乙酰胆碱酯酶抑制剂的色胺衍生物及其用途 |
| CN107118146B (zh) * | 2017-04-13 | 2019-09-03 | 宁波大学 | 一种6-溴色胺衍生物及其制备方法和用途 |
| DK3630098T3 (da) * | 2017-05-24 | 2021-04-26 | H Lundbeck As | Kombination af en 5-ht6-receptorantagonist og en acetylcholinsteraseinhibitor til anvendelse i behandlingen af alzheimers sygdom hos en patientsubpopulation som har apoe4-alleller |
| EA202190886A1 (ru) | 2018-09-28 | 2021-09-07 | Янссен Фармацевтика Нв | Модуляторы моноацилглицерин-липазы |
| TW202035409A (zh) | 2018-09-28 | 2020-10-01 | 比利時商健生藥品公司 | 單醯基甘油脂肪酶調節劑 |
| CN114555596A (zh) | 2019-09-30 | 2022-05-27 | 詹森药业有限公司 | 放射性标记的mgl pet配体 |
| NL2024431B1 (en) | 2019-12-11 | 2021-09-07 | Sulfateq Bv | Compounds for treatment of alzheimer’s disease |
| BR112022019077A2 (pt) | 2020-03-26 | 2022-12-27 | Janssen Pharmaceutica Nv | Moduladores da monoacilglicerol lipase |
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| FR2181559A1 (en) | 1972-04-28 | 1973-12-07 | Aec Chimie Organique Bio | N-Phenylalkyl-N-3-indolylalkyl-alkylamines - with sedative, neuroleptic, analgesic, hypotensive, antiserotonin, adrenolytic activity |
| JPS5764632A (en) | 1980-10-09 | 1982-04-19 | Mitsui Toatsu Chem Inc | Novel 2-arylethyl ether derivative and thioether derivative, their production and insecticide and acaricide |
| US5202336A (en) | 1986-09-24 | 1993-04-13 | Bayer Aktiengesellschaft | Antiflammatory quinolin methoxy phenylsulphonamides |
| DE3632329A1 (de) | 1986-09-24 | 1988-03-31 | Bayer Ag | Substituierte phenylsulfonamide |
| SE9103745D0 (sv) | 1991-12-18 | 1991-12-18 | Wikstroem Haakan | Aryl-triflates and related compounds |
| ATE167471T1 (de) | 1993-09-01 | 1998-07-15 | Allelix Biopharma | Tryptamin analoge mit 5-ht1d selektivität |
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| ATE346840T1 (de) | 1997-09-29 | 2006-12-15 | Aventis Pharma Inc | Aminoalkylphenol-derivate zur behandlung von depression und gedächtnis-funktionsstörung |
| GB9820113D0 (en) | 1998-09-15 | 1998-11-11 | Merck Sharp & Dohme | Therapeutic agents |
| DE69930308T2 (de) | 1998-12-11 | 2006-11-30 | Virginia Commonwealth University | Selektive 5-ht 6-rezeptor-liganden |
| KR20010086166A (ko) | 1999-01-13 | 2001-09-08 | 로즈 암스트롱, 크리스틴 에이. 트러트웨인 | 케모카인 수용체 조절제로서의 관능화된 헤테로시클 |
| US6750348B1 (en) | 1999-03-24 | 2004-06-15 | Anormed, Inc. | Chemokine receptor binding heterocyclic compounds |
| ES2566056T3 (es) | 2001-03-29 | 2016-04-08 | Eli Lilly And Company | N-(2-ariletil)bencilaminas como antagonistas del receptor 5-HT6 |
| RU2252936C2 (ru) | 2002-12-05 | 2005-05-27 | Институт физиологически активных веществ РАН | S-замещенные n-1-[(гетеро)арил]алкил-n`-[(гетеро)арил]алкилизотиомочевины, способ их получения, фармацевтическая композиция, способ изучения глутаматэргической системы, способы лечения (варианты) |
| PE20071143A1 (es) * | 2006-01-13 | 2008-01-20 | Wyeth Corp | Composicion farmaceutica que comprende un inhibidor de acetilcolinesterasa y un antagonista 5-hidroxitriptamina-6 |
| CN101500611A (zh) | 2006-06-23 | 2009-08-05 | 埃斯蒂维实验室股份有限公司 | 胆碱脂酶抑制剂与具有5-ht6受体亲和力的化合物的组合 |
| AR061637A1 (es) | 2006-06-26 | 2008-09-10 | Epix Delaware Inc | Composiciones y metodos de tratamiento de trastornos del snc |
| US20110098278A1 (en) * | 2009-07-23 | 2011-04-28 | Shire Llc | Galantamine amino acid and peptide prodrugs and uses thereof |
| TW201139370A (en) | 2009-12-23 | 2011-11-16 | Lundbeck & Co As H | Processes for the manufacture of a pharmaceutically active agent |
| JO3459B1 (ar) | 2012-09-09 | 2020-07-05 | H Lundbeck As | تركيبات صيدلانية لعلاج مرض الزهايمر |
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2013
- 2013-08-21 JO JOP/2013/0248A patent/JO3459B1/ar active
- 2013-09-06 BR BR112015005117-0A patent/BR112015005117B1/pt active IP Right Grant
- 2013-09-06 MX MX2015002879A patent/MX368305B/es active IP Right Grant
- 2013-09-06 KR KR1020207034028A patent/KR102342127B1/ko active IP Right Grant
- 2013-09-06 MY MYPI2015000575A patent/MY182539A/en unknown
- 2013-09-06 AP AP2015008306A patent/AP2015008306A0/xx unknown
- 2013-09-06 EA EA201590353A patent/EA030448B1/ru not_active IP Right Cessation
- 2013-09-06 RU RU2015107877A patent/RU2675786C2/ru active
- 2013-09-06 DK DK13759195.4T patent/DK2892563T3/en active
- 2013-09-06 CA CA2883751A patent/CA2883751C/en active Active
- 2013-09-06 GE GEAP201313752A patent/GEP201706776B/en unknown
- 2013-09-06 JP JP2015530420A patent/JP6693744B2/ja active Active
- 2013-09-06 TW TW102132182A patent/TWI632909B/zh active
- 2013-09-06 SI SI201331303T patent/SI2892563T1/sl unknown
- 2013-09-06 WO PCT/EP2013/068516 patent/WO2014037532A1/en active Application Filing
- 2013-09-06 AU AU2013311573A patent/AU2013311573B2/en active Active
- 2013-09-06 NZ NZ630589A patent/NZ630589A/en unknown
- 2013-09-06 LT LTEP13759195.4T patent/LT2892563T/lt unknown
- 2013-09-06 SG SG11201501774QA patent/SG11201501774QA/en unknown
- 2013-09-06 PL PL13759195T patent/PL2892563T3/pl unknown
- 2013-09-06 CN CN201380046768.6A patent/CN104619344A/zh active Pending
- 2013-09-06 EP EP13759195.4A patent/EP2892563B1/en active Active
- 2013-09-06 PT PT13759195T patent/PT2892563T/pt unknown
- 2013-09-06 ES ES13759195T patent/ES2703630T3/es active Active
- 2013-09-06 RS RS20181571A patent/RS58104B1/sr unknown
- 2013-09-06 KR KR1020157007345A patent/KR20150065680A/ko not_active IP Right Cessation
- 2013-09-09 US US14/021,033 patent/US9375418B2/en active Active
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2015
- 2015-02-23 IL IL237369A patent/IL237369B/en active IP Right Grant
- 2015-03-02 TN TNP2015000076A patent/TN2015000076A1/fr unknown
- 2015-03-06 CL CL2015000578A patent/CL2015000578A1/es unknown
- 2015-03-06 NI NI201500031A patent/NI201500031A/es unknown
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2016
- 2016-01-07 HK HK16100112.5A patent/HK1212217A1/xx unknown
- 2016-03-30 US US15/084,712 patent/US9687473B2/en active Active
- 2016-06-28 US US15/194,947 patent/US9789085B2/en active Active
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2017
- 2017-09-06 US US15/696,880 patent/US10660878B2/en active Active
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2018
- 2018-12-06 HR HRP20182069TT patent/HRP20182069T1/hr unknown
- 2018-12-06 JP JP2018228631A patent/JP2019059760A/ja active Pending
- 2018-12-21 CY CY181101390T patent/CY1121062T1/el unknown
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